| Cat.No. | Name | Information |
|---|---|---|
| M2347 | (+)-Bicuculline | (+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. |
| M5442 | Baclofen | Baclofen is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research. |
| M5653 | Flumazenil | Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses. |
| M14221 | THIP | THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist, functionally selective GABAAR ligand, exhibits agonism at α4β1δ, α4β3δ and weak antagonism at αβγ and α4β2δ GABAARs. |
| M14219 | NS11394 | NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. |
| M14218 | Etifoxine | Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents. |
| M14214 | γ-Aminobutyric acid | γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors). |
| M11530 | Guvacine | Guvacine, an alkaloid found in areca nut, is an effective inhibitor of GABA uptake. Guvacine inhibited rat GAT-1 with IC50 values of 39 μM, 58 μM and 378 μM, respectively. |
| M11353 | 6‴-Feruloylspinosin | 6‴-Feruloylspinosin is a flavonoid isolated from the seeds of Ziziphus jujuba. In rat hippocampal neurons, 6‴ -feruloylspinosin can cross the blood-brain barrier and enhance the mRNA expression of GABAAα1, GABAAα5 and GABABR1. |
| M11220 | 4-Aminobutyrate | |
| M10390 | Aminooxy-acetic acid | Aminooxy-acetic acid (AOA) is a GABA transaminase (GABA-T) inhibitor (Ki = 9.16 μM) that induces GABA accumulation in the brain. It also inhibits cystathionine β synthase (CBS) and cystathionine γ lyase (CSE) with IC50 values of 8.5 and 1.1 μM, respectively. Aminooxyacetic acid (Carboxymethoxylamine) is a malate-aspartate shuttle (MAS) inhibitor. |
| M10326 | Zuranolone | Zuranolone also known as SAGE-217, is a potent GABAA receptor agonist with EC50 values of 296 nM and 163 nM for α1β2γ2 and α4β3δ GABAA receptors. |
| M9874 | SSD114 hydrochloride | SSD114 hydrochloride is a GABAB receptor positive allosteric modulator. |
| M9856 | Pipequaline | Pipequaline (PK-8165) is a partial benzodiazepine receptor agonist with anxiolytic activity. |
| M9411 | AZD-7325 | AZD-7325 is a GABA-Aα2,3 -selective receptor modulator. |
| M9188 | Clomethiazole | Clomethiazole is a positive allosteric modulator at the barbiturate/picrotoxin site of the GABAA receptor. |
| M9127 | ONO-8590580 | ONO-8590580 is a GABAAα5 negative allosteric modulator which enhances long-term potentiation and improves cognitive deficits in preclinical models. |
| M9114 | LAU159 | LAU159 is a potent, functionally selective α6β3γ2 GABAA receptor modulator. |
| M8879 | Aminooxy-acetic acid (AOA) hemihydrochloride | Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T. |
| M8216 | Securinine | Securinine is an alkaloid widely in traditional folk medicine, it is a GABAA receptor antagonist. |
| M8027 | Brexanolone | Brexanolone (Allopregnanolone) is a positive allosteric modulator of GABAA chloride channel. |
| M7813 | Isoguvacine hydrochloride | Isoguvacine hydrochloride is a GABAA receptor agonist. |
| M7691 | Chlormethiazole hydrochloride | Chlormethiazole hydrochloride is a GABAA agonist; glycine receptor modulator. Clomethiazole hydrochloride is neuroprotective and prevents the degeneration of serotonergic nerve terminals induced by 3,4-methylenedioxymethamphetamine (MDMA). |
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